Comparison of toxicities of moxifloxacin, cefuroxime, and levofloxacin to corneal endothelial cells in vitro

J Cataract Refract Surg. 2014 Nov;40(11):1872-8. doi: 10.1016/j.jcrs.2014.08.027. Epub 2014 Sep 26.

Abstract

Purpose: To evaluate and compare the toxic effects of moxifloxacin, cefuroxime, and levofloxacin on human corneal endothelial cells in vitro and determine the safe intracameral concentrations for them.

Setting: Tottori University, Tottori, Japan.

Design: Experimental study.

Methods: Human corneal endothelial cells in culture were exposed to moxifloxacin, cefuroxime, and levofloxacin at concentrations up to 2000 μg/mL. Evaluation of membrane damage was determined by ethidium homodimer-1 uptake and cell viability, by intrinsic esterase activity. The inhibitory effects of the 3 antibiotics on the constitutive secretion of interleukin-6 (IL-6) by human corneal endothelial cells were determined by enzyme-linked immunosorbent assay.

Results: The acute effects (6 hour) of the 3 antibiotics on membrane damage and cell death were dose-dependent for moxifloxacin and levofloxacin (≥ 500 μg/mL). For cefuroxime, membrane damage was not observed at 6 hours and only slight damage was detected at 24 hours at concentrations higher than 500 μg/mL. The half maximum inhibitory concentrations on cell viability of moxifloxacin, levofloxacin, and cefuroxime were 487 μg/mL, 578 μg/mL, and 1600 μg/mL, respectively. The inhibitory effects of the 3 antibiotics on the constitutive secretion of IL-6 were observed at 15.6 μg/mL or higher, indicating the antibiotics can impair the secretion of the protective cytokine even at low concentrations.

Conclusions: Moxifloxacin at more than 500 μg/mL caused damage to the cell membranes of corneal endothelial cells; even higher concentrations decreased cell viability. Considering the lower minimum inhibitory concentration for inhibiting 90% growth by moxifloxacin, intracameral moxifloxacin at 500 μg/mL or less is recommended for prophylactic use.

Financial disclosure: Dr. Inoue is a medical advisor to Alcon Japan Ltd. No author has a financial or proprietary interest in any material or method mentioned.

Publication types

  • Comparative Study

MeSH terms

  • Anti-Bacterial Agents / toxicity*
  • Cefuroxime / toxicity*
  • Cell Survival
  • Cells, Cultured
  • Dose-Response Relationship, Drug
  • Endothelium, Corneal / drug effects*
  • Endothelium, Corneal / metabolism
  • Enzyme-Linked Immunosorbent Assay
  • Fluoroquinolones / toxicity*
  • Humans
  • Inhibitory Concentration 50
  • Interleukin-6 / metabolism
  • Levofloxacin / toxicity*
  • Moxifloxacin

Substances

  • Anti-Bacterial Agents
  • Fluoroquinolones
  • IL6 protein, human
  • Interleukin-6
  • Levofloxacin
  • Cefuroxime
  • Moxifloxacin